1. Cell Cycle/DNA Damage Apoptosis
  2. DNA/RNA Synthesis Apoptosis
  3. BLM-IN-2

BLM-IN-2 is a Bloom's Syndrome Protein (BLM) inhibitor with an IC50 value of 0.8 μM. BLM-IN-2 effectively suppresses the proliferation, invasion, cell cycle arrest and apoptosis of CRC cells. BLM-IN-2 can be used for the reserarch of colorectal cancer (CRC).

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BLM-IN-2

BLM-IN-2 Chemical Structure

CAS No. : 3037604-86-4

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Description

BLM-IN-2 is a Bloom's Syndrome Protein (BLM) inhibitor with an IC50 value of 0.8 μM. BLM-IN-2 effectively suppresses the proliferation, invasion, cell cycle arrest and apoptosis of CRC cells. BLM-IN-2 can be used for the reserarch of colorectal cancer (CRC)[1].

IC50 & Target

IC50: 0.8 μM (BLM)[1]

Cellular Effect
Cell Line Type Value Description References
HCT-116 IC50
0.6 μM
Compound: 21
Inhibition of colony formation in human HCT-116 cells incubated for 10 days by crystal violet staining based assay
Inhibition of colony formation in human HCT-116 cells incubated for 10 days by crystal violet staining based assay
[PMID: 36459756]
HCT-116 IC50
1 μM
Compound: 21
Inhibition of cell invasion in human HCT-116 cells incubated for 48 hrs by crystal violet staining based transwell assay
Inhibition of cell invasion in human HCT-116 cells incubated for 48 hrs by crystal violet staining based transwell assay
[PMID: 36459756]
HCT-116 IC50
1.9 μM
Compound: 21
Antiproliferative activity against wild type human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by propidium iodide staining based high-content imaging analysis
Antiproliferative activity against wild type human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by propidium iodide staining based high-content imaging analysis
[PMID: 36459756]
HCT-116 IC50
2.8 μM
Compound: 21
Cytotoxicity against human HCT-116 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay
Cytotoxicity against human HCT-116 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay
[PMID: 36459756]
NCM460 IC50
15.6 μM
Compound: 21
Cytotoxicity against human NCM460 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay
Cytotoxicity against human NCM460 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay
[PMID: 36459756]
RKO IC50
0.7 μM
Compound: 21
Inhibition of colony formation in human RKO cells incubated for 10 days by crystal violet staining based assay
Inhibition of colony formation in human RKO cells incubated for 10 days by crystal violet staining based assay
[PMID: 36459756]
RKO IC50
5.4 μM
Compound: 21
Cytotoxicity against human RKO cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay
Cytotoxicity against human RKO cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay
[PMID: 36459756]
SW480 IC50
0.6 μM
Compound: 21
Inhibition of colony formation in human SW480 cells incubated for 10 days by crystal violet staining based assay
Inhibition of colony formation in human SW480 cells incubated for 10 days by crystal violet staining based assay
[PMID: 36459756]
SW480 IC50
2.2 μM
Compound: 21
Cytotoxicity against human SW480 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay
Cytotoxicity against human SW480 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay
[PMID: 36459756]
In Vitro

BLM-IN-2 (0-20 μM) has good inhibitory effect on BLM unwinding and binding DNA with IC50 values of 0.8 μM and 2.3 μM, respectively[1].
BLM-IN-2 exhibits the potent BLM-dependent cytotoxicity against the CRC cells but weak against normal cells[1].
BLM-IN-2 (3 μM; 48 h) disrupts the HRR level while inhibiting BLM located on the DSB site and trigger DNA damage in the CRC cells[1].
BLM-IN-2 (0-5 μM; 48 h) effectively suppresses the proliferation and invasion of CRC cells, along with cell cycle arrest and apoptosis[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: HCT116 cells; HCT116, SW480 and RKO cells
Concentration: 0-5 μM; 0.5, 1, 2 μM
Incubation Time: 48 h; 10 days
Result: Induced proliferation arrest.
Completely inhibited the growth of cancer cells at the concentration around 2 μM, had a good anti-CRC activity.

Apoptosis Analysis[1]

Cell Line: HCT116, SW480 and RKO cells
Concentration: 1 μM
Incubation Time: 48 h
Result: Induced apoptosis and necrosis in HCT116, SW480 and RKO.

Cell Cycle Analysis[1]

Cell Line: HCT116, SW480 and RKO cells
Concentration: 4 μM
Incubation Time: 48 h
Result: Changed the cell proportion of the S or G2/M phase in CRC cells, arrested the cell cycle at the S phase in HCT116 and SW480 and arrested the cell cycle of HCT116, SW480 and RKO at the G2/M phase.

Cell Invasion Assay[1]

Cell Line: HCT116 cells
Concentration: 0.25, 0.5, 1, 2, 4 μM
Incubation Time: 48 h
Result: Obviously decreased the invasion in HCT116 cells with an IC50 value of 1.0 μM and had inhibitory on CRC invasion.
Molecular Weight

605.58

Formula

C33H38BrFN4O

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CCN(CCCNC1=C(C=C2C(N(C(/C=C/C3=CC=C(C=C3)C(C)C)=NC2=C1)CC4=CC=C(C=C4)Br)=O)F)CC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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Product Name:
BLM-IN-2
Cat. No.:
HY-151939
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